Cefpirome
Based on 1 publication(s) in Google Scholar
Cefpirome (HR-810) is a cephalosporin antibiotic that can cross cell membranes and the blood-brain barrier. Cefpirome binds to penicillin-binding proteins with high affinity, thereby inhibiting bacterial cell wall synthesis. Cefpirome exhibits bactericidal and growth-inhibitory activities against Gram-negative bacteria, Gram-positive bacteria, and susceptible anaerobic bacteria (including some β-lactamase-producing strains).
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- No. CAS: 84957-29-9
- Fòrmula: C22H22N6O5S2
- Peso molecular:514.58
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications Citing Use of MedChemExpress (MCE) Cefpirome
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Actividad biológica
Descripciòn
IC50 & Target
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β-lactam |
In Vitro
Cefpirome exhibits excellent in vitro antibacterial activity against most Enterobacteriaceae, methicillin (HY-121544)-sensitive staphylococci and streptococci, moderate activity against Pseudomonas aeruginosa, variable activity against anaerobes, and weak activity against methicillin-resistant staphylococci and Enterococcus faecalis[1].
Cefpirome is stable to most plasmid-mediated and chromosome-mediated β-lactamases, except for extended-spectrum SHV enzymes, and retains activity against β-lactamase-producing, third-generation cephalosporin-resistant Enterobacteriaceae strains[1].
Cefpirome exhibits rapid outer membrane permeability to Gram-negative bacteria, and has a high-affinity binding capacity to key penicillin-binding proteins in both Gram-negative and Gram-positive bacteria, which endows it with broad-spectrum antibacterial activity[1].
Cefpirome (18 h) prevented the emergence of Enterobacter cloacaemutants at a concentration of 1 μg/mL, thereby defining a narrow mutant selection window between the MIC (0.125 μg/mL) and the mutant prevention concentration[2].
Cefpirome (0.06-32 μg/mL; 18-24 h) potently inhibits clinically isolated strains of Enterobacteriaceae, with MIC90 ≤ 0.5 μg/mL for most species. It exhibits activity against non-glucose-fermenting Gram-negative bacilli, as well as both Oxacillin (HY-B0925A)-susceptible and Oxacillin-resistant staphylococci (the MIC90 is 1 μg/mL for Oxacillin-susceptible Staphylococcus aureus and 16 μg/mL for Oxacillin-resistant Staphylococcus aureus). Only a slight salt-dependent increase in MIC is observed for coagulase-negative staphylococci[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Cefpirome (0.025-1.56 mg/kg) demonstrates high in vivo efficacy against a range of bacterial systemic infections in mice, with ED50 values ranging from 0.025 to 1.56 mg/kg[1].
Cefpirome shows in vivo activity against Pseudomonas aeruginosa-induced systemic infection in mice, but is approximately 2-fold less potent than ceftazidime[1].
Cefpirome exhibits in vivo efficacy against Acinetobacter spp.-induced systemic infection in mice[1].
Cefpirome (15.4 mg/kg) is highly bactericidal against Klebsiella pneumoniae-induced pneumonia in mice, with an ED50 of 15.4 mg/kg at 18 hours[1].
Cefpirome (0.4-50 mg/kg b.i.d.; intramuscular injection; every 12 hours; 18 days) results in dose-dependent survival of rats with K. pneumoniae pneumonia and only minimal selection of stable derepressed ampD-mutated E. cloacae mutants from intestinal flora[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:RP/AEur/RijHsd rats (male, 11-15 weeks old, 250-350 g, left-sided unilateral pneumonia induced via tracheal cannulation with Klebsiella pneumoniae ATCC 43816)[2]
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Dosage:0.4 mg/kg b.i.d.; 0.8 mg/kg b.i.d.; 1.6 mg/kg b.i.d.; 3.1 mg/kg b.i.d.; 6.3 mg/kg b.i.d.; 12.5 mg/kg b.i.d.; 25 mg/kg b.i.d.; 50 mg/kg b.i.d.
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Administration:intramuscular injection; every 12 hours; 18 days
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Result:Dose-dependently reduced the number of target bacteria. However, in a few rats that received higher doses of treatment, stable drug-resistant mutant strains were detected, but their numbers were generally low or showed a downward trend.
Ensayo clínico
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 84957-29-9
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Peso molecular 514.58
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Fòrmula C22H22N6O5S2
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SMILES
O=C1[C@@H](NC(/C(C2=CSC(N)=N2)=N\OC)=O)[C@@]3([H])SCC(C[N+]4=CC=CC5=C4CCC5)=C(C([O-])=O)N13
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Synonyms
HR 810
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (1)
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Journal Impact Factor
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Most Recent
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Biomed Res Int
In Vitro Activity of β-Lactams in Combination with β-Lactamase Inhibitors against Mycobacterium tuberculosis Clinical Isolates. [Abstract]2018 Jul 2:2018:3579832. PMID: 30065936
Pureza y Documentación
Referencias
[1].
Wiseman LR, et al. A review of its antibacterial activity, pharmacokinetic properties and clinical efficacy in the treatment of severe nosocomial infections and febrile neutropenia. Drugs. 1997 Jul;54(1):117-40.
[Content Brief]
[2].
Gautam V, et al. Cefpirome Treatment Results in Limited Selection of Stable Derepressed Enterobacter cloacae Mutants in the Intestinal Flora of Rats Treated for an Experimental Klebsiella pneumoniae Pulmonary Infection. Microb Drug Resist. 2020 Apr;26(4):341-348.
[Content Brief]
[3]. Bertram MA, et al. In vitro activity of HR 810, a new cephalosporin. Antimicrob Agents Chemother. 1984;26(2):277-279. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Keywords
- Cefpirome
- 84957-29-9
- HR 810
- HR810
- HR-810
- Antibiotic
- Bacterial
- Penicillin-binding protein (PBP)
- Enterobacter cloacae
- Gram-negative bacteria
- mouse models of pneumonia
- bacterial cell wall synthesis
- anaerobic bacteria
- mouse models of systemic infection
- Klebsiella pneumoniae
- penicillin binding proteins
- Pseudomonas aeruginosa
- Gram-positive bacteria
- Inhibitor
- inhibitor
- inhibit